Real-time and automated monitoring of antischistosomal drug activity profiles for screening of compound libraries
| Autor: | Paolo S. Ravaynia, Stefan Biendl, Francesco Grassi, Jennifer Keiser, Andreas Hierlemann, Mario M. Modena |
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| Rok vydání: | 2021 |
| Předmět: | |
| Zdroj: | iScience, 25 (4) |
| ISSN: | 2589-0042 |
| Popis: | Schistosomiasis is a neglected tropical disease that affects over 200 million people annually. As the antischistosomal drug pipeline is currently empty, repurposing of compound libraries has become a source for accelerating drug development, which demands the implementation of high-throughput and efficient screening strategies. Here, we present a parallelized impedance-based platform for continuous and automated viability evaluation of Schistosoma mansoni schistosomula in 128 microwells during 72 h to identify antischistosomal hits in vitro. By initially screening 57 repurposed compounds against larvae, five drugs are identified, which reduce parasite viability by more than 70%. The activity profiles of the selected drugs are then investigated via real-time dose-response monitoring, and four compounds reveal high potency and rapid action, which renders them suitable candidates for follow-up tests against adult parasites. The study shows that our device is a reliable tool for real-time drug screening analysis of libraries to identify new promising therapeutics against schistosomiasis. iScience, 25 (4) ISSN:2589-0042 |
| Databáze: | OpenAIRE |
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